RS-17053 [Ligand Id: 495] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL88272 (RS-17053)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
  • Alpha-1a adrenergic receptor in Bovine [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
  • Alpha-1a adrenergic receptor in Rabbit [ChEMBL: CHEMBL3637] [UniProtKB: O02824]
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  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
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  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
ChEMBL Binding affinity was tested on human Alpha-1A adrenergic receptor B 9.2 pKi 0.63 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
ChEMBL Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active B 9.22 pKi 0.6 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 657-664 [PMID:15664832]
GtoPdb - - 9.3 pKi - - - Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248];
FEBS Lett (1998) 422: 279-83 [PMID:9490024];
Eur J Pharmacol (1999) 370: 337-43 [PMID:10334511];
Mol Pharmacol (1996) 49: 209-15 [PMID:8632751]
Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
ChEMBL In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor B 9.1 pKi 0.79 nM Ki J. Med. Chem. (1997) 40: 2674-2687 [PMID:9276013]
Alpha-1a adrenergic receptor in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3637] [UniProtKB: O02824]
ChEMBL Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay F 7.3 pKd 50.12 nM Kd J. Med. Chem. (1997) 40: 2674-2687 [PMID:9276013]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL Binding affinity was tested on human Alpha-1B adrenergic receptor B 7.8 pKi 15.85 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL Binding affinity was tested on human Alpha-1D adrenergic receptor B 7.8 pKi 15.85 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
GtoPdb - - 7.8 pKi - - - Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]